溶剂蒸发法制备波洛沙姆-凝胶固体分散体;一种提高替硝唑溶解度的有效方法

S. Ahirrao, Durgesh Kale, D. Bhambere, Dinesh Kuber
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引用次数: 0

摘要

许多BCS II类和IV类药物具有很高的治疗潜力,但由于溶解性差,生物利用度较低。因此,目前的研究重点是提高难溶性药物的溶解度和溶出率;磺甲硝咪唑。采用不同的方法,用凝胶和波洛沙姆制备替硝唑固体分散体;揉捏、熔融和溶剂蒸发。通过饱和溶解度、药物含量、体外溶出度、红外光谱(FTIR)、DSC、XRD和稳定性研究对制剂进行评价。优化的凝胶和波洛沙姆固体分散体的溶出速度比纯药物快。体外溶出度研究表明,制剂Sg14批的释药率为94.43%,相关系数(R²)为0.949;制剂Sp14批的释药率为97.69%,相关系数(R²)为0.993。DSC研究表明,药物与载体之间没有相互作用,而优化制剂批次的XRD研究表明,与纯药物替硝唑的XRD图谱相比,结晶度明显降低。替硝唑的溶解度和体外溶出率发生显著变化是由于在优化的制剂批次中保持了非晶态。因此,本研究工作的总体配方和评价研究表明,溶剂蒸发法固体分散是提高替硝唑溶解度的有效手段。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Poloxamer and gelucire solid dispersion prepared by solvent evaporation; an effective means for solubility enhancement of tinidazole
Many BCS Class II and IV drugs possess high therapeutic potential but shows less bioavailability due to poor solubility. Hence present study is focused on improvement of solubility and dissolution rate of poorly soluble drug; tinidazole. Solid dispersion of tinidazole were prepared with gelucire and poloxamer using various methods; kneading, fusion and solvent evaporation. Formulations were evaluated by saturation solubility, drug content, in vitro dissolution rate, FTIR, DSC, XRD and stability study. Optimised solid dispersions of gelucire and poloxamer provided dissolution rates faster than that of pure drug. In vitro dissolution studies revealed that formulation batch Sg14 shows 94.43 percent drug release with a correlation coefficient (R²) of 0.949 and batch Sp14 shows 97.69 percent drug release with a correlation coefficient (R²) of 0.993. DSC study revealed that there was no interaction between drug and carrier whereas the XRD study of optimised formulation batches demonstrates that there was a significant decrease in crystallinity when compared with XRD pattern of pure drug tinidazole. Significant change in solubility and in vitro dissolution rate of tinidazole would be due to amorphous state maintained in the optimised formulation batches. Hence overall formulation and evaluation studies of present research work indicate that solid dispersion by solvent evaporation method is an effective means to improve the solubility of tinidazole.
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